Target intelligence / Profile preview

Arginine vasopressin receptor 1A (AVPR1A or V1A receptor)

Target
AVPR1A or V1A receptor
Molecular classification
G protein-coupled receptor, Membrane receptor, Peptide receptor, Receptor
01

Overview

Arginine vasopressin receptor 1A (AVPR1A, V1A receptor) is a G protein-coupled receptor found predominantly in vascular smooth muscle, platelets, liver, myometrium, and brain. Its principal endogenous ligand is vasopressin (antidiuretic hormone). The receptor mediates vasopressor (vasoconstrictor) effects via activation of phosphatidyl-inositol-calcium signaling through Gq proteins, resulting in increased intracellular calcium and smooth muscle contraction. AVPR1A is also involved in platelet aggregation, regulation of arterial blood pressure, uterine contraction, and various social and behavioral processes. Clinically, V1A receptor ligands are important in cardiovascular management (e.g., vasopressin and terlipressin for shock) and are explored in the context of neuropsychiatric and social behavior-related research. Overactivity can cause hypertension and thrombosis, while genetic polymorphisms in the gene are linked to variability in social behavior and mating in humans.

Other names
Vasopressin V1a receptorV1-vascular vasopressin receptorAntidiuretic hormone receptor 1AAVPR1Vascular/hepatic-type arginine vasopressin receptor
02

Mechanism of action

Agonists stimulate vasoconstriction via Gq-protein activation. Antagonists block receptor-mediated vasoconstriction and related effects. Indirect effects on blood pressure, platelet aggregation, and uterine contraction.

03

Biological functions

VasoconstrictionSignal transductionPlatelet aggregationGlycogenolysisUterine contractionCalcium-mediated signalingBlood circulationCellular response to hormone stimulusRegulation of systemic arterial blood pressureSocial behavior
04

Disease associations

Cardiovascular disease (shock, hypertension)ThrombosisBehavioral and neuropsychiatric conditionsReproductive disordersOther (linked to social and mating behavior via genetic polymorphisms)
05

Safety considerations

Excessive vasoconstriction (risk of hypertension, ischemia of non-vital organs)Thrombosis (due to increased platelet aggregation)Potential behavioral effects with drugs modulating central AVPR1AOff-target vasopressor effects during therapy
06

Interacting drugs

Vasopressin (agonist)

6 more in the full profile.

07

Biomarkers

AVPR1A gene polymorphisms (linked to behavioral phenotypes)Changes in blood pressure and platelet function as pharmacodynamic markersNo widely used specific clinical biomarkers for AVPR1A in patient selection

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